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Orodispersible tablets obtained by compression molding

a technology of orodispersible tablets and compression molding, which is applied in the field of pharmaceuticals, can solve the problems of limiting the industrial development of orodispersible tablets, affecting the quality of orodispersible tablets,

Active Publication Date: 2018-10-30
ETHYPHARM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text discusses the results of studies that found that when orodispersible tablets are made with certain ingredients and a certain process, they have better strength and can be easier to chew. This text is important for those working on making these tablets and improving their quality.

Problems solved by technology

To allow rapid disintegration, orodispersible tablets have a porous structure and are compressed at lower pressures than conventional tablets, the drawbacks being that they may be more fragile and difficult to handle.
However, there are still at the present time certain characteristics that limit the industrial development of orodispersible tablets, especially their excessive friability and their occasionally unpleasant taste and mouthfeel.
Thus, although orodispersible tablets remain a fairly widespread form that patients appreciate, especially for their practical and rapid use, a study performed by the Applicant has shown that the taste and mouthfeel of a tablet appear to be the most important parameters for patients, and thus the unpleasant taste and / or unpleasant mouthfeel are one of the major causes of non-compliance with medical treatments, and thus of their failure.
However, this direct compression method is not always entirely satisfactory, especially in terms of the friability and the disintegration time of the tablets thus obtained.

Method used

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  • Orodispersible tablets obtained by compression molding
  • Orodispersible tablets obtained by compression molding
  • Orodispersible tablets obtained by compression molding

Examples

Experimental program
Comparison scheme
Effect test

example 1 (comparative)

FT” by Direct Compression

[0133]Materials and Methods

[0134]The starting materials used in the ODT FTs are indicated in table 1.

[0135]

TABLE 1NamesManufacturerFunctionNeutrals 500 / 600NP PharmAP mimicPearlitol ® SD 200 and 160CRoquetteDiluentPolyplasdone ® XLISPDisintegrantAspartameAjimotoSweetenerSyloid ® 244 FPGrace DavisonFlow agentMagnesium stearatePeter GrevenLubricant

[0136]The preparation of the mixtures is performed in a Lodige type FM 50 E machine (ploughshare granulator) and then in Frogerais 27 or 60 L cubic mixers.

[0137]Drying is performed in a Binder APT.line™ FP oven equipped with perforated trays.

[0138]The mixture is compressed on a Fette P1200 rotary press equipped with mechanical feed assistance.

[0139]The mass, thickness and hardness of the tablets are controlled on a Checkmaster 4 Fette machine.

[0140]The friability is measured on an Erweka TA 10 machine according to the method described in the European Pharmacopea (edition 7, chapter 2.9.7.).

[0141]The in vitro disintegr...

example 2

[0159]The starting materials used are indicated in table 5 below.

[0160]

TABLE 5NamesManufacturerFunctionNeutrals 500 / 600NP PharmAP mimicMannitol 60RoquetteDiluentPolyplasdone ® XLISPDisintegrantAspartameAjimotoSweetenerSyloid ® 244 FPGrace DavisonFlow agentAerosil ® R 972EvonikFlow agentL-HPC LH 21SeppicBinder and disintegrantPruv ®JRS PharmaHydrophilic lubricantAerosil ® 200EvonikFlow agentGum arabicCarlo ErbaBinderGelucire ® 44 / 14GattefosséHumectantAcDiSol ®FMC BiopolymerDisintegrantExplotab ®JRS PharmaDisintegrant

[0161]The machines used are the same as those described in example 1 above.

[0162]The mixture in the form of grains is prepared in a Lodige machine and the excipients for compression are then added as an external phase (Syloid®, Aerosil®, Pruv®) with the Neutrals 500 / 600. This mixture is compressed using 12 mm punches (round, flat, beveled type).

[0163]The target hardness values of 50 and 70 N are targeted for each test.

[0164]For each type of tablet obtained, the mass, thic...

example 3

[0208]Tablets according to the invention are prepared, using Syloid 244FP as flow agent both in the wet excipient grains and directly in the mixture for compression.

[0209]Tables 15 and 16 below represent, respectively, the percentage composition of the wet mixture of excipients, in the form of wet grains, and that of the mixture for compression.

[0210]

TABLE 15NamesPercentages (dry extract)PercentagesMannitol 6071.1469.59Polyplasdone XL17.8517.46Aspartame3.363.29L-HPC LH 216.316.17Syloid 244FP1.341.31Water2.22Total100.00100

[0211]

TABLE 16NamesPercentagesNeutrals 500 / 60020.09Wet mixture of excipients (in the form of grains)76.00Syloid 244FP1.95Pruv ®1.95Total100.00

[0212]Table 17 below represents the residual humidity values measured for the wet mixture of excipients in the form of grains and for the mixture for compression, the compositions of which are given in tables 15 and 16, respectively.

[0213]

TABLE 17LOD (%)KF (%)Mixture of wet excipients3.02.9Mixture for compression2.62.7

[0214]Ta...

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Abstract

Embodiments of the present invention provide an orodispersible tablet having a hardness of 30 to 80 N, and preferably 40 to 75 N, a brittleness less than 1% and preferably less than 0.5%, disintegrating in the mouth within 60 seconds and preferably within 40 seconds, comprising an active ingredient in the form of coated microcrystals or microgranules and a mixture of excipients chosen from a group comprising a diluent, a disintegrant, a sweetener, a binder, a levelling agent, a humectant or wetting agent, a lubricant, a flavoring agent, a dye, and mixtures thereof, said mixture of excipients preferably coming in the form of grains.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a U.S. National Phase Application of International Application No. PCT / FR2013 / 053113, filed Dec. 17, 2013, which claims the benefit of priority of French Application No. 12 62175, filed Dec. 17, 2012, the contents of which applications are incorporated by reference herein, in their entireties and for all purposes.FIELD OF THE INVENTION[0002]The present invention relates to the field of pharmacy, and more particularly to that of galenic.[0003]The subject of the invention is an orodispersible tablet obtained by compression molding.BACKGROUND OF THE INVENTION[0004]An orodispersible tablet is a solid form that disintegrates or dissolves in the mouth, solely on contact with saliva, generally in less than 60 seconds.[0005]Orodispersible tablets are a galenical form that is on the rise, which has greatly developed in recent years. The reason for this is that orodispersible tablets have many advantages and are particularly sui...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K9/20A61K9/16A61K9/00A61K45/06
CPCA61K9/0056A61K9/1623A61K9/205A61K9/2009A61K9/2013A61K45/06A61K9/2027A61K9/2054A61K9/2077A61K9/2081A61K9/2095A61K9/2018
Inventor DECORTE, ISABELLEGENDROT, EDOUARDPREVOST, YANN
Owner ETHYPHARM SA